GRL-142
GRL-142 is a potent HIV-1 protease inhibitor capable of crossing the blood-brain barrier. GRL-142 exhibits extremely high inhibitory activity against both wild-type and multidrug-resistant strains (IC50=0.0094 nM). GRL-142 acts synergistically with the P2/P2' segments via a unique scaffold binding mechanism, utilizes fluorine-mediated stable interactions to maintain its bioactive conformation, adapts to p51 HIV-1 protease mutants, and maintains the flap-closed state by directly acting on the flap tip residues. GRL-142 disrupts the flap-water hydrogen bond network of wild-type protease, thereby effectively blocking viral replication. GRL-142 can be used to study HIV-1 infection and the associated neurocognitive disorder (HAND).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Formel: C34H40F2N4O7S2
- Molecular Weight:718.83
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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HIV-1 |
GRL-142 exhibits ultra-potent inhibitory activity against wild-type HIV-1 (Ki=14 pM), and maintains high activity against most drug-resistant HIV-1 strains, but shows a significant reduction in activity against highly drug-resistant p51 strains (with a maximum reduction of 436-fold)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 718.83
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Formel C34H40F2N4O7S2
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SMILES
[H][C@]1(C2CO[C@@]3(OCC4(C23)CC41)[H])OC(N[C@H]([C@@H](CN(S(=O)(C5=CC6=C(N=C(S6)NC7CC7)C=C5)=O)CC(C)C)O)CC8=CC(F)=CC(F)=C8)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
GRL-142 Related Classifications
HY-181888 Related Classifications
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- GRL-142
- GRL142
- GRL 142
- HIV
- HIV Protease
- flap-tip residue
- flap-water hydrogen bonding networks
- p51 HIV-1 protease variant
- drug-resistant HIV-1 strains
- blood-brain barrier
- HIV-associated neurocognitive disorders
- S2/S2' subsites
- multidrug-resistant HIV-1 protease
- HIV-1 infection
- wild-type HIV-1 protease
- Inhibitor
- inhibitor
- inhibit